| 摘要 |
Imidazo 2,1-b benzoxazole- 3-acetamide derivs. of formula (I) and their acid addition salts are new. X = H, halogen, 1-3C alkyl, or 1-3C alkoxy; Y = H, halogen, or 1-3C alkyl; R1 = H or methyl; R2 = H or methyl. The compounds may be given enterally or parenterally at a daily dosage of 1-1000 mg. EXAMPLE 22.6 g 2,2-diethoxy- N,N-dimethyl acetamide and 3.5 ml 37% HCl in 140 ml acetic acid were stirred at 50 deg.C for 1 hour then 13 g sodium acetate and 12.3 g (II; X = Y = H) was added and the mixture stirred at the same temperature for 2.5 hours. The mixture was evaporated and the residue dissolved in water and dichloromethane, filtered, and the organic phase separated, dried and purified to give 10.2 g (IV; X = Y = H; R1 = R2 = methyl), m.pt. 153-155 deg C. 2.73 g (IV) was treated with 10 ml thionyl chloride in 60 ml dichloromethane at ambient temperature for 15 hours. Excess thionyl chloride was removed, to give 2.5 g (V.HCl; Hal = Cl; X = Y = H; R1 = R2 = methyl). This was reduced with 2.92 g Rongalite (RTM) in 80 ml dichloromethane for 16 hours at ambient temperature, and purified to give 0.9g (I; X = H; R1 = R2 = methyl) m.pt. 190-192 deg C.
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